No

Calcium Channel Blocker

Management of essential hypertension

C

Clinical effects on the fetus: Crosses the placenta; may exhibit tocolytic effect

Breast-feeding/lactation: No data available

Hypersensitivity to nicardipine or any component; advanced aortic stenosis

Blood pressure lowering should be done at a rate appropriate for the patient's condition. Rapid drops in blood pressure can lead to arterial insufficiency. Use with caution in CAD (can cause increase in angina), CHF (can worsen heart failure symptoms), and pheochromocytoma (limited clinical experience). Peripheral infusion sites (for I.V. therapy) should be changed ever 12 hours. Titrate I.V. dose cautiously in patients with CHF, renal, or hepatic dysfunction. Use the I.V. form cautiously in patients with portal hypertension (can cause increase in hepatic pressure gradient). Safety and efficacy have not been demonstrated in pediatric patients. Abrupt withdrawal may cause rebound angina in patients with CAD.

1% to 10%:

Cardiovascular: Flushing (6% to 10%), palpitations (3.3% to 4%), tachycardia (1% to 3.4%), peripheral edema (dose-related 7% to 8%), increased angina (dose-related 5.6%)

Central nervous system: Headache (6.4% to 8%), dizziness (4% to 7%), somnolence (4.2% to 6%), paresthesia (1%)

Dermatologic: Rash (1.2%)

Gastrointestinal: Nausea (1.9% to 2.2%), dry mouth (1.4%)

Neuromuscular & skeletal: Weakness (4.2% to 6%), myalgia (1%)

<1% (Limited to important or life-threatening symptoms): Abnormal EKG, insomnia, malaise, abnormal dreams, vomiting, constipation, nocturia, tremor, nervousness, malaise, dyspnea, gingival hyperplasia, syncope, sustained tachycardia

Case report: Parotitis

The primary cardiac symptoms of calcium blocker overdose include hypotension and bradycardia. The hypotension is caused by peripheral vasodilation, myocardial depression, and bradycardia. Bradycardia results from sinus bradycardia, second- or third-degree atrioventricular block, or sinus arrest with junctional rhythm. Intraventricular conduction is usually not affected so QRS duration is normal (verapamil does prolong the P-R interval and bepridil prolongs the Q-T and may cause ventricular arrhythmias, including torsade de pointes).

In a few reported cases, overdose with calcium channel blockers has been associated with hypotension and bradycardia, initially refractory to atropine but becoming more responsive to this agent when larger doses (approaching 1 g/hour for more than 24 hours) of calcium chloride was administered.

CYP3A3/4 enzyme substrate

Calcium may reduce the calcium channel blocker's effects, particularly hypotension.

Cyclosporine's serum concentrations are increased by nicardipine; avoid this combination. Use another calcium channel blocker or monitor cyclosporine trough levels and renal function closely.

Nafcillin decreases plasma concentration of nicardipine; avoid this combination.

Protease inhibitor like amprenavir and ritonavir may increase nicardipine's serum concentration.

Rifampin increases the metabolism of the calcium channel blocker; adjust the dose of the calcium channel blocker to maintain efficacy.

Compatible with D₅W, D₅1/2 NS, D₅NS, and D₅W with 40 mEq potassium chloride; 0.45% and 0.9% NS; do not mix with 5% sodium bicarbonate and lactated Ringer's solution; store at room temperature; protect from light; stable for 24 hours at room temperature

Inhibits calcium ion from entering the "slow channels" or select voltage-sensitive areas of vascular smooth muscle and myocardium during depolarization, producing a relaxation of coronary vascular smooth muscle and coronary vasodilation; increases myocardial oxygen delivery in patients with vasospastic angina

Onset of action: Oral: 1-2 hours; I.V.: 10 minutes

Duration: 2-6 hours

Absorption: Oral: Well absorbed, ~100%

Protein binding: 95%

Metabolism: Extensive first-pass metabolism; only metabolized in the liver

Bioavailability: Absolute, 35%

Half-life: 2-4 hours

Time to peak: Peak serum levels occur within 20-120 minutes and an onset of hypotension occurs within 20 minutes

Elimination: As metabolites in urine

Adults:

Immediate release: Initial: 20 mg 3 times/day; usual: 20-40 mg 3 times/day (allow 3 days between dose increases)

Sustained release: Initial: 30 mg twice daily, titrate up to 60 mg twice daily

I.V. (dilute to 0.1 mg/mL): Initial: 5 mg/hour increased by 2.5 mg/hour every 15 minutes to a maximum of 15 mg/hour

Dosing adjustment in renal impairment: Titrate dose beginning with 20 mg 3 times/day (immediate release) or 30 mg twice daily (sustained release).

Dosing adjustment in hepatic impairment: Starting dose: 20 mg twice daily (immediate release) with titration.

Equivalent oral vs I.V. infusion doses:

20 mg q8h oral, equivalent to 0.5 mg/hour I.V. infusion

30 mg q8h oral, equivalent to 1.2 mg/hour I.V. infusion

40 mg q8h oral, equivalent to 2.2 mg/hour I.V. infusion

Alcohol: Avoid use

Nicardipine alone or in combination with other agents is effective in the management of hypertension and angina. Nicardipine should be used with caution in patients with heart failure.

Drowsiness and dizziness are common; may rarely cause insomnia

Concurrent use with propranolol may increase AV nodal effects

No information available to require special precautions

Other drugs of this class can cause gingival hyperplasia (ie, nifedipine). The first case of nicardipine-induced gingival hyperplasia has been reported in a child taking 40-50 mg daily for 20 months

Take as directed; do not alter dosage regimen or increase, decrease, or discontinue without consulting prescriber. Do not crush or chew tablets or capsules. Take with nonfatty food. Avoid caffeine and alcohol. Consult prescriber before increasing exercise routine (decreased angina does not mean it is safe to increase exercise). Change position slowly to prevent orthostatic events. May cause dizziness or fatigue; use caution when driving or engaging in tasks that require alertness until response to drug is known. Frequent small meals, frequent mouth care, sucking lozenges, or chewing gum may reduce nausea. Report swelling, difficulty breathing or new cough, unresolved fatigue, unusual weight gain, or unresolved dizziness. Pregnancy/breast-feeding precautions: Inform prescriber if you are or intend to be pregnant. Breast-feeding is not recommended.

Monitor closely for orthostasis; ampuls must be diluted before use; do not crush sustained release product; to assess adequacy of blood pressure response, measure blood pressure 8 hours after dosing

Caplet: 20 mg, 30 mg

Sustained release: 30 mg, 45 mg, 60 mg

Injection: 2.5 mg/mL (10 mL)

Pascual-Castroviejo I and Pascual Pascual SI, "Nicardipine-Induced Gingival Hyperplasia," Neurologia, 1997, 12(1):37-9.